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Polymer-metal complex composite having MRI contrast ability and MRI contrasting and/or antitumor composition using the same

Foreign code F110005825
File No. AF12-02WO
Posted date Oct 19, 2011
Country United States of America
Application number 200913000836
Gazette No. 20110123458
Gazette No. 8961949
Date of filing Jun 26, 2009
Gazette Date May 26, 2011
Gazette Date Feb 24, 2015
International application number JP2009061772
International publication number WO2009157561
Date of international filing Jun 26, 2009
Date of international publication Dec 30, 2009
Priority data
  • P2008-167823 (Jun 26, 2008) JP
  • 2009WO-JP61772 (Jun 26, 2009) WO
Title Polymer-metal complex composite having MRI contrast ability and MRI contrasting and/or antitumor composition using the same
Abstract (US8961949)
The present invention provides a polymer-metal complex composite, which comprises a block copolymer capable of serving as a constituent member of a polymeric micelle and a metal complex having MRI contrast ability, accumulates in a tumor-specific manner, achieves high image contrast even in a small amount, and has reduced side effects and a long retention time in blood.
The polymer-metal complex composite of the present invention comprises a block copolymer (A) represented by general formula (a) and a metal complex (B) having MRI contrast ability, wherein the composite comprises a structure in which a carboxyl anion of poly(carbo) in the copolymer (A) is attached to the metal complex (B) via a metal atom (M).
Scope of claims [claim1]
1. A polymer-metal complex composite, which comprises a block represented by the following general formula (1) or (2):
wherein R1 represents a hydrogen atom or an unsubstituted or substituted linear or branched C1-12 alkyl group, L1 and L2 each represent a linker group, R2 independently represents a methylene group or an ethylene group, R3 independently represents a hydrogen atom, a protecting group for an amino group, a hydrophobic group or a polymerizable group, R4 represents a hydroxyl group or an initiator residue, R5 independently represents a hydrogen atom, an alkali metal ion, or a group represented by the following general formula (3) and/or (4):
wherein R6 represents a metal atom or a group derived from a metal complex, and R7 represents a group derived from a metal complex having MRI contrast ability,
provided that at least one R5 comprises the group represented by general formula (3) in which each R6 is independently a group derived from a metal complex having antitumor activity represented by the following formula (5-a) or (6-a):
each R7 is independently a group represented by the following formula (7-a), (8-a), (9-a) or (10-a):
m represents an integer of 5 to 20,000, n represents an integer of 2 to 5,000, and x represents an integer of 0 to 5,000provided that x <= n.
[claim2]
2. The composite according to claim 1, which is represented by the following general formula (1-a) or (2-a):
[claim3]
3. The composite according to claim 1 or 2, wherein the group represented by general formula (3) is independently a group represented by the following formula (15-a), (16-a), (17-a) or (18-a):
[claim4]
4. The composite according to claim 1, which when dispersed in an aqueous medium forms micellar particles.
[claim5]
5. The composite according to claim 4, which has an average dispersed particle size of 10 nm to 1 mu m in an aqueous medium, as measured by dynamic light scattering.
[claim6]
6. An MRI contrasting and antitumor composition, which comprises the composite according to claim 1.
[claim7]
7. An MRI contrasting method for tumor detection, which comprises administering the composite according to claim 1 to the body of an animal subject.
[claim8]
8. An MRI contrasting and antitumor kit, which comprises the composite according to claim 1.
[claim9]
9. The composite according to claim 1 or 2, wherein the group represented by general formula (3) is independently a group represented by the following formula (11-a), (12-a), (13-a), or (14-a):
  • Inventor, and Inventor/Applicant
  • KATAOKA KAZUNORI
  • KAIDA SACHIKO
  • CABRAL HORACIO
  • KUMAGAI MICHIAKI
  • SEKINO MASAKI
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
Reference ( R and D project ) CREST Establishment of Innovative Manufacturing Technology Based on Nanoscience AREA
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